Tolcapone

TASMAR

Open Tolcapone in the interactive console ↗

Pronunciation: TOEL-ka-poen

Tolcapone ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Tolcapone ballicule

Tolcapone TASMAR mascot mnemonic cartoon — Visual mnemonic: Tolcapone mascot
**“Total Capone Taskbar”**

What it isCentral and peripheral catechol-O-methyltransferase inhibitor used with levodopa/carbidopa for Parkinson disease with motor fluctuations.

Why this oneCrosses the blood-brain barrier and extends levodopa effect more strongly than peripheral-only COMT inhibitors.

What limits itRequires normal liver tests, written consent, and LFTs every 2–4 weeks for 6 months; worst diarrhea of the class.

Pearls

Withdrawn in Canada and elsewhere for fatal hepatotoxicity.
Unlike entacapone, need not be timed with each levodopa dose.

Tolcapone molecular structure (skeletal formula) — Molecular structure: Tolcapone

Tolcapone prescription history

Animated chart of estimated U.S. prescriptions per year, Parkinson medicines (1948–2026). Tolcapone enters in 1998 (estimated).

FDA-approved for

Parkinson disease with motor fluctuations (1998)

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability1 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk1 / 4

Legacy pregnancy categoryUnknown / historical label unavailable

Defining liabilityOrthostasis, hallucinations, dyskinesia and impulse-control symptoms; abrupt withdrawal can be hazardous.

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Risk of potentially fatal acute fulminant liver failure; reserve for fluctuating Parkinson's not responding to other adjuncts; withdraw if no benefit within 3 weeks; do not initiate with liver disease or ALT/AST >2x ULN.

FDA dosing	Population	Start	Target	Max
Parkinson's disease (adjunct to levodopa/carbidopa)	Adult	100 mg TID	100 mg TID	200 mg TID

Renal Undefined

Hepatic Contraindicated in liver disease; do not initiate if ALT/AST >2x ULN

Instructions

Only prescribe with concomitant carbidopa/levodopa.
Withdraw if no substantial clinical benefit within 3 weeks.
Do not retreat patients withdrawn for hepatocellular injury.

Available strengths

tab 100 mg

Contraindications

Liver disease
Prior tolcapone-induced hepatocellular injury (withdrawn from drug)
History of nontraumatic rhabdomyolysis or hyperpyrexia and confusion possibly medication-related

Cautions

Hepatocellular injury / fulminant liver failure - monitor LFTs
Rhabdomyolysis
Use caution with severe dyskinesia or dystonia
Events reported with dopaminergic therapy (hallucinations, hypotension)

Adverse reactions

Severe hepatocellular injury incl. fatal fulminant liver failure
Elevated ALT/AST

Pregnancy No adequate human data; animal embryo-fetal toxicity; given with levodopa/carbidopa (teratogenic in rabbits)

Lactation Undefined

Cost

Tolcapone (TASMAR)

Strength		#/mo	generic $/mo	CostPlus
100 mg	tab	90 TID		out of stock

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Tolcapone is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2015

Open Tolcapone in the interactive console ↗